Rasarfin is a novel dual Ras and ARF6 inhibitor, selectively inhibits small G proteins Ras and ARF6 with IC50 of 7 and 0.7 uM.
Rasarfin blocks agonist-mediated internalization of AT1R and other GPCRs.
Rasarfin also potently inhibits agonist-induced ERK1/2 signaling by GPCRs, and MAPK and Akt signaling by EGFR, as well as prevents cancer cell proliferation.
Rasarfin blocks GPCR internalization through inhibition of ARF6, a regulator of CCV-mediated endocytosis, and receptor-mediated MAPK.
